Moxifloxacin-gelrite In Situ ophthalmic gelling system against photodynamic therapy for treatment of bacterial corneal inflammation
- 334 Downloads
In this study, six in situ gelling formulations based on Gelrite were prepared and evaluated for the retained ophthalmic delivery of Moxifloxacin (Mox). The effectiveness of the best developed formula G5 was compared with photodynamic therapy (PDT), the recent expanding approach for the treatment of ophthalmologic disorders after the assessment of optimum photodynamic inactivation parameters that permit efficient pathogens eradication. It was found that, Staphylococcus aureus (S. aureus) (Gram-positive) was more susceptible to effective lethal photosensitization that reaches 93.5% reduction in viable count than Escherichia coli (E. coli) (Gramnegative) of 76.1% using 3 mg/mL Hematoporphyrin (HP), illuminated by 630 nm Light Emitting Diode (LED) at 9 J/cm2 and incubated for 15 min. Following topical instillation of G5 to rabbits corneas, higher amount of Mox was retained in the aqueous humor up to 24 h with significant 6-fold increase in the Cmax and AUC(0-∞) compared to vigamox® commercial eye drops. After post corneal infection with S. aureus, both approaches were effectively treating the infection without causing ocular irritation or collateral damage to corneal tissue where G5 showed remarkable improvement after four days compared to seven days of PDT treatment.
Key wordsMoxifloxacin Ocular delivery In situ gelling systems Gelrite® Photodynamic therapy
Unable to display preview. Download preview PDF.
- Bajaj, I. B., Survase, S. A., Saudagar, P. S., and Singhal, R. S., Gellan gum: fermentative production, downstream processing and applications. Food Technol. Biotechnol., 45, 341–354 (2007).Google Scholar
- Borchard, G., Lueßen, H. L., de Boer, A. G., Verhoef, J. C., Lehr, C.-M., and Junginger, H. E., The potential of mucoadhesive polymers in enhancing intestinal peptide drug absorption. III: Effects of chitosan-glutamate and carbomer on epithelial tight junctions in vitro. J. Control. Release, 39, 131–138 (1996).CrossRefGoogle Scholar
- El-Adly, A. A., Photoactive anionic porphyrin derivative against Gram-positive and Gram-negative bacteria. J. Appl. Sci. Res., 4, 1817–1821 (2008).Google Scholar
- Hamblin, M. R., O’Donnell, D. A., Murthy, N., Rajagopalan, K., Michaud, N., Sherwood, M. E., and Hasan, T., Polycationic photosensitizer conjugates: effects of chain length and Gram classification on the photodynamic inactivation of bacteria. J. Antimicrob. Chemother., 49, 941–951 (2002).PubMedCrossRefGoogle Scholar
- Lembo, A. J., Ganz, R. A., Sheth, S., Cave, D., Kelly, C., Levin, P., Kazlas, P. T., Baldwin, P. C., 3rd, Lindmark, W. R., McGrath, J. R., and Hamblin M. R., Treatment of Helicobacter pylori infection with intra-gastric violet light phototherapy: a pilot clinical trial. Lasers Surg. Med., 41, 337–344 (2009).PubMedCrossRefGoogle Scholar
- Sensoy, D., Cevher, E., Sarici, A., Yilmaz, M., Ozdamar, A., and Bergisşadi, N., Bioadhesive sulfacetamide sodium microspheres: evaluation of their effectiveness in the treatment of bacterial keratitis caused by Staphylococcus aureus and Pseudomonas aeruginosa in a rabbit model. Eur. J. Pharm. Biopharm., 72, 487–495 (2009).PubMedCrossRefGoogle Scholar
- Torkildsen, G. and O’Brien, T. P., Conjunctival tissue pharmacokinetic properties of topical azithromycin 1% and moxifloxacin 0.5% ophthalmic solutions: a single-dose, randomized, open-label, active-controlled trial in healthy adult volunteers. Clin. Ther., 30, 2005–2014 (2008).PubMedCrossRefGoogle Scholar